Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding
説明 | GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding |
In vitro | GSK805 inhibits the expression of IL-17 (at 0.5 μM) in na?ve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells[1]. |
In vivo | GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction[1]. |
細胞研究 | CD4+CD62LhighCD25? naive CD4+ T cells were purified by FACS sorting following a MACS bead isolation of CD4+ cells. Naive CD4+ cells were activated with plate-bound anti-CD3 (2 μg/ml) and anti-CD28 (2 μg/ml). For Th17 cell differentiation, cultures were supplemented with IL-6 (20 ng/ml) plus TGF-β1 (1 ng/ml), and IL-23 (10 ng/ml) was added after 48 h. RORγt inhibitors or vehicle control DMSO was also included in the cultures. After 96 h, cells were collected for further experiments[1]. |
分子量 | 532.36 |
分子式 | C23H18Cl2F3NO4S |
CAS No. | 1426802-50-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (187.84 mM)
You can also refer to dose conversion for different animals. 詳細
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GSK805 1426802-50-7 Metabolism ROR GSK 805 immunity RAR-related orphan receptor Inhibitor inhibit oral CNS penetrant Th17 cell GSK-805 inhibitor